Table 10.
Physicochemical properties and in vitro binding and metabolism
| Cmpd | 37 | 1a |
| MW | 323 | 415 |
| Log D 7.4 | 2.8b | 4.0c |
| Solubility (μg/mL) | ||
| FaSSGF (pH 1.6) | 46.4 | 6.8 |
| FaSSIF (pH 6.5) | 60.1 | 5.1 |
| FeSSIF (pH 5.8) | 115 | 27.6 |
| PBS (pH 7.4) | 45.6 | 2.0 |
| H/R/M plasma protein binding (% bound) | 90.0 / 88.2 / 88.9 | 99.9 / 97.0 / 99.7 |
| Albumax binding (% bound) | 51.8 | 83.1 |
| Microsome binding (% bound) | 29.9 | 71.7 |
| DMEM/10% FCS binding (% bound) | 31.5 | 78.5 |
| H/R/M CLint (μL/min/mg) | 10 / 14 / 24 | <7 / <7 / <7 |